research use only

Tacrolimus monohydrate phosphatase inhibitor

Name: Tacrolimus monohydrate
Brand: Selleck Chemicals
SKU: S5788
Availability: InStock
Rating: 5 (6 reviews)

Cat.No.S5788

Tacrolimus monohydrate (Tacrolimus, FK506) is a macrolide antibiotic that primarily acts as an inhibitor of calcineurin phosphatase by binding to FK506 binding protein (FKBP). This inhibition blocks calcium-dependent processes, including interleukin-2 gene transcription, nitric oxide synthase activation, cell degranulation, and apoptosis, and also has immunosuppressive, neuroregenerative and neuroprotective properties.

Chemical Structure

Molecular Weight: 822.04

Jump to

Quality Control

Batch: S578801 DMSO]100 mg/mL]false]Ethanol]100 mg/mL]false]Water]Insoluble]false Purity: 99.404%

Cited in Nature Medicine for its top-tier quality
COA
NMR
SDS/MSDS
Datasheet

99.404

Related Targets	Dehydrogenase HSP Transferase P450 (e.g. CYP17) PDE PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism Casein Kinase
Other phosphatase Inhibitors	Osunprotafib (ABBV-CLS-484) SHP099 Hydrochloride RMC-4550 SHP099 Batoprotafib (TNO155) GSK2830371 β-Glycerophosphate sodium salt hydrate NSC87877 TPI-1 Suramin sodium salt

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (121.64 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (6.08mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.500mg/ml (3.04mM)	Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	822.04	Formula	C₄₄H₆₉NO₁₂.H₂O	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	109581-93-3	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent

Read more about storage stability stock solution CAS number

Mechanism of Action

Targets/IC₅₀/Ki	calcineurin phosphatase
References	[1] https://pubmed.ncbi.nlm.nih.gov/8588225/ [2] https://pubmed.ncbi.nlm.nih.gov/15198862/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-09-04)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT07524530	NOT_YET_RECRUITING	Core Binding Factor Alpha Subunits; Hematologic Neoplasms; Leukemia; Lymphoma	National Cancer Institute (NCI)	2026-09-09	PHASE2
NCT05646992	RECRUITING	Uterine Factor Infertility	Johns Hopkins University	2023-03-01	PHASE2; PHASE3
NCT04877288	RECRUITING	Renal Allograft Recipients	Bristol-Myers Squibb	2021-07-21	PHASE3
NCT06291103	NOT_YET_RECRUITING	Kidney Transplant Rejection	University Hospital, Rouen	2026-07-01	PHASE2; PHASE3
NCT05031897	RECRUITING	Acute Lymphoblastic Leukemia; Acute Myeloid Leukemia; Adult T-Cell Leukemia/Lymphoma; Aplastic Anemia; Chronic Lymphocytic Leukemia; Chronic Myeloid Leukemia, BCR-ABL1 Positive; Chronic Myelomonocytic Leukemia; Essential Thrombocythemia; Hematopoietic and Lymphatic System Neoplasm; Hodgkin Lymphoma; Multiple Myeloma; Myelodysplastic Syndrome; Myelofibrosis; Myeloid Neoplasm; Non-Hodgkin Lymphoma; Polycythemia Vera; Small Lymphocytic Lymphoma	Thomas Jefferson University	2021-10-25	PHASE2
NCT05027945	RECRUITING	Immunodeficiency; Hematopoietic Stem Cell Transplantation	National Cancer Institute (NCI)	2023-02-23	PHASE2

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):